Details of the Target

General Information of Target

Target ID LDTP08061
Target Name Cytochrome P450 2U1 (CYP2U1)
Gene Name CYP2U1
Gene ID 113612
Synonyms
Cytochrome P450 2U1; Long-chain fatty acid omega-monooxygenase; EC 1.14.14.80
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSSPGPSQPPAEDPPWPARLLRAPLGLLRLDPSGGALLLCGLVALLGWSWLRRRRARGIP
PGPTPWPLVGNFGHVLLPPFLRRRSWLSSRTRAAGIDPSVIGPQVLLAHLARVYGSIFSF
FIGHYLVVVLSDFHSVREALVQQAEVFSDRPRVPLISIVTKEKGVVFAHYGPVWRQQRKF
SHSTLRHFGLGKLSLEPKIIEEFKYVKAEMQKHGEDPFCPFSIISNAVSNIICSLCFGQR
FDYTNSEFKKMLGFMSRGLEICLNSQVLLVNICPWLYYLPFGPFKELRQIEKDITSFLKK
IIKDHQESLDRENPQDFIDMYLLHMEEERKNNSNSSFDEEYLFYIIGDLFIAGTDTTTNS
LLWCLLYMSLNPDVQEKVHEEIERVIGANRAPSLTDKAQMPYTEATIMEVQRLTVVVPLA
IPHMTSENTVLQGYTIPKGTLILPNLWSVHRDPAIWEKPEDFYPNRFLDDQGQLIKKETF
IPFGIGKRVCMGEQLAKMELFLMFVSLMQSFAFALPEDSKKPLLTGRFGLTLAPHPFNIT
ISRR
Target Bioclass
Enzyme
Family
Cytochrome P450 family
Subcellular location
Endoplasmic reticulum membrane
Function
A cytochrome P450 monooxygenase involved in the metabolism of arachidonic acid and its conjugates. Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (CPR; NADPH-ferrihemoprotein reductase). Acts as an omega and omega-1 hydroxylase for arachidonic acid and possibly for other long chain fatty acids. May modulate the arachidonic acid signaling pathway and play a role in other fatty acid signaling processes. May down-regulate the biological activities of N-arachidonoyl-serotonin, an endocannabinoid that has anti-nociceptive effects through inhibition of fatty acid amide hydrolase FAAH, TRPV1 receptor and T-type calcium channels. Catalyzes C-2 oxidation of the indole ring of N-arachidonoyl-serotonin forming a less active product 2-oxo-N-arachidonoyl-serotonin.
Uniprot ID
Q7Z449
Ensemble ID
ENST00000332884.11
HGNC ID
HGNC:20582
ChEMBL ID
CHEMBL4523986

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CCK81 SNV: p.L446M .
KASUMI2 SNV: p.I96V .
MCC26 SNV: p.D452N .
NCIH1155 SNV: p.M325V .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K487(6.53)  LDD0277  [1]
Jackson_14
 Probe Info  		3.33  LDD0123  [2]
Acrolein
 Probe Info  		N.A.  LDD0221  [3]
DBIA
 Probe Info  		C490(0.94)  LDD1508  [4]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
OEA-DA
 Probe Info  		20.00  LDD0046  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0215  AC10 HEK-293T C490(0.94)  LDD1508  [4]
 LDCM0226  AC11 HEK-293T C490(0.96)  LDD1509  [4]
 LDCM0237  AC12 HEK-293T C490(1.00)  LDD1510  [4]
 LDCM0259  AC14 HEK-293T C490(0.96)  LDD1512  [4]
 LDCM0277  AC18 HEK-293T C490(1.07)  LDD1516  [4]
 LDCM0278  AC19 HEK-293T C490(0.98)  LDD1517  [4]
 LDCM0279  AC2 HEK-293T C490(0.91)  LDD1518  [4]
 LDCM0280  AC20 HEK-293T C490(1.02)  LDD1519  [4]
 LDCM0281  AC21 HEK-293T C490(0.96)  LDD1520  [4]
 LDCM0282  AC22 HEK-293T C490(0.99)  LDD1521  [4]
 LDCM0286  AC26 HEK-293T C490(1.00)  LDD1525  [4]
 LDCM0287  AC27 HEK-293T C490(0.88)  LDD1526  [4]
 LDCM0288  AC28 HEK-293T C490(1.08)  LDD1527  [4]
 LDCM0289  AC29 HEK-293T C490(0.95)  LDD1528  [4]
 LDCM0290  AC3 HEK-293T C490(1.01)  LDD1529  [4]
 LDCM0291  AC30 HEK-293T C490(0.96)  LDD1530  [4]
 LDCM0295  AC34 HEK-293T C490(0.96)  LDD1534  [4]
 LDCM0296  AC35 HEK-293T C490(0.95)  LDD1535  [4]
 LDCM0297  AC36 HEK-293T C490(0.90)  LDD1536  [4]
 LDCM0298  AC37 HEK-293T C490(1.06)  LDD1537  [4]
 LDCM0299  AC38 HEK-293T C490(1.10)  LDD1538  [4]
 LDCM0301  AC4 HEK-293T C490(0.96)  LDD1540  [4]
 LDCM0304  AC42 HEK-293T C490(1.04)  LDD1543  [4]
 LDCM0305  AC43 HEK-293T C490(0.84)  LDD1544  [4]
 LDCM0306  AC44 HEK-293T C490(0.98)  LDD1545  [4]
 LDCM0307  AC45 HEK-293T C490(0.95)  LDD1546  [4]
 LDCM0308  AC46 HEK-293T C490(1.03)  LDD1547  [4]
 LDCM0312  AC5 HEK-293T C490(0.79)  LDD1551  [4]
 LDCM0313  AC50 HEK-293T C490(0.99)  LDD1552  [4]
 LDCM0314  AC51 HEK-293T C490(0.89)  LDD1553  [4]
 LDCM0315  AC52 HEK-293T C490(0.91)  LDD1554  [4]
 LDCM0316  AC53 HEK-293T C490(0.83)  LDD1555  [4]
 LDCM0317  AC54 HEK-293T C490(1.04)  LDD1556  [4]
 LDCM0321  AC58 HEK-293T C490(0.95)  LDD1560  [4]
 LDCM0322  AC59 HEK-293T C490(0.84)  LDD1561  [4]
 LDCM0323  AC6 HEK-293T C490(0.98)  LDD1562  [4]
 LDCM0324  AC60 HEK-293T C490(1.05)  LDD1563  [4]
 LDCM0325  AC61 HEK-293T C490(0.95)  LDD1564  [4]
 LDCM0326  AC62 HEK-293T C490(0.97)  LDD1565  [4]
 LDCM0248  AKOS034007472 HEK-293T C490(0.99)  LDD1511  [4]
 LDCM0367  CL1 HEK-293T C490(1.42)  LDD1571  [4]
 LDCM0368  CL10 HEK-293T C490(1.65)  LDD1572  [4]
 LDCM0369  CL100 HEK-293T C490(1.20)  LDD1573  [4]
 LDCM0370  CL101 HEK-293T C490(1.04)  LDD1574  [4]
 LDCM0372  CL103 HEK-293T C490(0.87)  LDD1576  [4]
 LDCM0373  CL104 HEK-293T C490(1.10)  LDD1577  [4]
 LDCM0374  CL105 HEK-293T C490(1.16)  LDD1578  [4]
 LDCM0376  CL107 HEK-293T C490(0.87)  LDD1580  [4]
 LDCM0377  CL108 HEK-293T C490(0.96)  LDD1581  [4]
 LDCM0378  CL109 HEK-293T C490(1.33)  LDD1582  [4]
 LDCM0381  CL111 HEK-293T C490(1.17)  LDD1585  [4]
 LDCM0382  CL112 HEK-293T C490(1.14)  LDD1586  [4]
 LDCM0383  CL113 HEK-293T C490(1.05)  LDD1587  [4]
 LDCM0385  CL115 HEK-293T C490(0.97)  LDD1589  [4]
 LDCM0386  CL116 HEK-293T C490(1.15)  LDD1590  [4]
 LDCM0387  CL117 HEK-293T C490(1.22)  LDD1591  [4]
 LDCM0389  CL119 HEK-293T C490(0.91)  LDD1593  [4]
 LDCM0391  CL120 HEK-293T C490(1.07)  LDD1595  [4]
 LDCM0392  CL121 HEK-293T C490(1.10)  LDD1596  [4]
 LDCM0394  CL123 HEK-293T C490(1.24)  LDD1598  [4]
 LDCM0395  CL124 HEK-293T C490(1.07)  LDD1599  [4]
 LDCM0396  CL125 HEK-293T C490(1.16)  LDD1600  [4]
 LDCM0398  CL127 HEK-293T C490(0.92)  LDD1602  [4]
 LDCM0399  CL128 HEK-293T C490(1.02)  LDD1603  [4]
 LDCM0400  CL13 HEK-293T C490(1.02)  LDD1604  [4]
 LDCM0402  CL15 HEK-293T C490(0.95)  LDD1606  [4]
 LDCM0403  CL16 HEK-293T C490(0.99)  LDD1607  [4]
 LDCM0405  CL18 HEK-293T C490(1.03)  LDD1609  [4]
 LDCM0406  CL19 HEK-293T C490(1.06)  LDD1610  [4]
 LDCM0408  CL20 HEK-293T C490(1.22)  LDD1612  [4]
 LDCM0409  CL21 HEK-293T C490(1.06)  LDD1613  [4]
 LDCM0410  CL22 HEK-293T C490(1.26)  LDD1614  [4]
 LDCM0413  CL25 HEK-293T C490(1.39)  LDD1617  [4]
 LDCM0415  CL27 HEK-293T C490(0.89)  LDD1619  [4]
 LDCM0416  CL28 HEK-293T C490(1.19)  LDD1620  [4]
 LDCM0418  CL3 HEK-293T C490(1.22)  LDD1622  [4]
 LDCM0419  CL30 HEK-293T C490(1.00)  LDD1623  [4]
 LDCM0420  CL31 HEK-293T C490(1.21)  LDD1624  [4]
 LDCM0421  CL32 HEK-293T C490(1.11)  LDD1625  [4]
 LDCM0422  CL33 HEK-293T C490(1.28)  LDD1626  [4]
 LDCM0423  CL34 HEK-293T C490(1.89)  LDD1627  [4]
 LDCM0426  CL37 HEK-293T C490(1.06)  LDD1630  [4]
 LDCM0428  CL39 HEK-293T C490(0.79)  LDD1632  [4]
 LDCM0429  CL4 HEK-293T C490(1.37)  LDD1633  [4]
 LDCM0430  CL40 HEK-293T C490(0.98)  LDD1634  [4]
 LDCM0432  CL42 HEK-293T C490(1.00)  LDD1636  [4]
 LDCM0433  CL43 HEK-293T C490(1.01)  LDD1637  [4]
 LDCM0434  CL44 HEK-293T C490(1.03)  LDD1638  [4]
 LDCM0435  CL45 HEK-293T C490(0.87)  LDD1639  [4]
 LDCM0436  CL46 HEK-293T C490(1.40)  LDD1640  [4]
 LDCM0439  CL49 HEK-293T C490(1.21)  LDD1643  [4]
 LDCM0443  CL52 HEK-293T C490(1.14)  LDD1646  [4]
 LDCM0445  CL54 HEK-293T C490(1.27)  LDD1648  [4]
 LDCM0446  CL55 HEK-293T C490(0.98)  LDD1649  [4]
 LDCM0447  CL56 HEK-293T C490(1.20)  LDD1650  [4]
 LDCM0448  CL57 HEK-293T C490(1.06)  LDD1651  [4]
 LDCM0449  CL58 HEK-293T C490(1.50)  LDD1652  [4]
 LDCM0451  CL6 HEK-293T C490(1.31)  LDD1654  [4]
 LDCM0453  CL61 HEK-293T C490(1.04)  LDD1656  [4]
 LDCM0455  CL63 HEK-293T C490(0.87)  LDD1658  [4]
 LDCM0456  CL64 HEK-293T C490(1.49)  LDD1659  [4]
 LDCM0458  CL66 HEK-293T C490(1.09)  LDD1661  [4]
 LDCM0459  CL67 HEK-293T C490(1.03)  LDD1662  [4]
 LDCM0460  CL68 HEK-293T C490(1.51)  LDD1663  [4]
 LDCM0461  CL69 HEK-293T C490(1.15)  LDD1664  [4]
 LDCM0462  CL7 HEK-293T C490(1.30)  LDD1665  [4]
 LDCM0463  CL70 HEK-293T C490(1.17)  LDD1666  [4]
 LDCM0466  CL73 HEK-293T C490(1.33)  LDD1669  [4]
 LDCM0469  CL76 HEK-293T C490(0.96)  LDD1672  [4]
 LDCM0471  CL78 HEK-293T C490(1.03)  LDD1674  [4]
 LDCM0472  CL79 HEK-293T C490(1.05)  LDD1675  [4]
 LDCM0473  CL8 HEK-293T C490(1.50)  LDD1676  [4]
 LDCM0474  CL80 HEK-293T C490(1.07)  LDD1677  [4]
 LDCM0475  CL81 HEK-293T C490(1.06)  LDD1678  [4]
 LDCM0476  CL82 HEK-293T C490(1.30)  LDD1679  [4]
 LDCM0479  CL85 HEK-293T C490(1.15)  LDD1682  [4]
 LDCM0481  CL87 HEK-293T C490(1.01)  LDD1684  [4]
 LDCM0482  CL88 HEK-293T C490(1.13)  LDD1685  [4]
 LDCM0484  CL9 HEK-293T C490(1.22)  LDD1687  [4]
 LDCM0485  CL90 HEK-293T C490(1.34)  LDD1688  [4]
 LDCM0486  CL91 HEK-293T C490(1.13)  LDD1689  [4]
 LDCM0487  CL92 HEK-293T C490(1.22)  LDD1690  [4]
 LDCM0488  CL93 HEK-293T C490(1.19)  LDD1691  [4]
 LDCM0489  CL94 HEK-293T C490(1.40)  LDD1692  [4]
 LDCM0492  CL97 HEK-293T C490(1.24)  LDD1695  [4]
 LDCM0494  CL99 HEK-293T C490(1.01)  LDD1697  [4]
 LDCM0495  E2913 HEK-293T C490(1.06)  LDD1698  [4]
 LDCM0468  Fragment33 HEK-293T C490(1.02)  LDD1671  [4]
 LDCM0107  IAA HeLa N.A.  LDD0221  [3]
 LDCM0016  Ranjitkar_cp1 MDA-MB-231 3.33  LDD0123  [2]

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
2 Appendage and Scaffold Diverse Fully Functionalized Small-Molecule Probes via a Minimalist Terminal Alkyne-Aliphatic Diazirine Isocyanide. J Org Chem. 2018 Sep 21;83(18):11245-11253. doi: 10.1021/acs.joc.8b01831. Epub 2018 Aug 31.
3 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
4 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402
5 Mapping Protein Targets of Bioactive Small Molecules Using Lipid-Based Chemical Proteomics. ACS Chem Biol. 2017 Oct 20;12(10):2671-2681. doi: 10.1021/acschembio.7b00581. Epub 2017 Sep 20.
Mass spectrometry data entry: PXD007570